Topical ophthalmological compositions

Abstract

A topical ophthalmological composition includes a therapeutically effective amount of a muscarinic receptor antagonist as an active pharmaceutical ingredient; and a semifluorinated alkane, as a liquid vehicle. The topical ophthalmological composition treats an ocular disease.

1 . A topical ophthalmological composition comprising:
 a therapeutically effective amount of a muscarinic receptor antagonist as an active pharmaceutical ingredient; and   a semifluorinated alkane, as a liquid vehicle. wherein the topical ophthalmological composition treats an ocular disease.   
     
     
         2 . The topical ophthalmological composition of  claim 1 , wherein the muscarinic receptor antagonist is selected from the group consisting of atropine, pirenzepine, aclidinium bromide, benztropine, cyclopentolate, diphenhydramine, doxylamine, dimenhydrinate, dicyclomine, darifenacin, flavoxate, hydroxyzine, ipratropium, mebeverine, oxybutynin, procyclidine, scopolamine, solifenacin, tropicamide, tiotropium, trihexyphenidyl, and tolterodine. 
     
     
         3 . The topical ophthalmological composition of  claim 2 , wherein the muscarinic receptor antagonist is atropine. 
     
     
         4 . The topical ophthalmological composition of  claim 3 , wherein the atropine is in a free base form or a salt form. 
     
     
         5 . The topical ophthalmological composition of  claim 4 , wherein the concentration of the atropine in a free base form is from about 0.0001% to about 1.0% (w/w), preferably, from about 0.001% to about 0.1% (w/w), more preferably, about 0.01% to about 0.1% (w/w). 
     
     
         6 . The topical ophthalmological composition of  claim 1 , wherein the semifluorinated alkane is a compound of formula RFRH or of formula RFRHRF, wherein RF is a perfluorinated hydrocarbon with 15 or less carbon atoms, and wherein RH is a non-fluorinated hydrocarbon with 15 or less carbon atoms. 
     
     
         7 . The topical ophthalmological composition of  claim 6 , wherein the semifluorinated alkane is selected from the group consisting of F4H5, F4H6, F6H4, F6H6, F6H8 and F6H10. 
     
     
         8 . The topical ophthalmological composition of  claim 7 , wherein the semifluorinated alkane is F6H8 (perfluorohexyloctane). 
     
     
         9 . The topical ophthalmological composition of  claim 1 , further comprising an organic cosolvent selected from the group consisting of phenylethyl alcohol, ethanol, isopropanol, glycerol, propylene glycol, and polyethylene glycol. 
     
     
         10 . The topical ophthalmological composition of  claim 9 , wherein the organic cosolvent is ethanol or phenylethyl alcohol. 
     
     
         11 . The topical ophthalmological composition of  claim 10 , wherein the concentration of ethanol is about 1% (w/w) or less; or the concentration of phenylethyl alcohol is about 1% (w/w) or less. 
     
     
         12 . The topical ophthalmological composition of  claim 1 , wherein the topical ophthalmological composition is a non-aqueous solution, a suspension, or an emulsion. 
     
     
         13 . The topical ophthalmological composition of  claim 12 , wherein the atropine in the topical ophthalmological composition is chemically stable for at least 0.5 year, for at least 1 year, or for at least 2 years. 
     
     
         14 . The topical ophthalmological composition of  claim 1 , wherein the topical ophthalmological composition is adapted for topically administering as eye drops to an eye of a patient. 
     
     
         15 . The topical ophthalmological composition of  claim 14 , wherein the topical ophthalmological composition is adapted to cause minimal irritation in the eye. 
     
     
         16 . The topical ophthalmological composition of  claims 1 , wherein the composition is for the treatment of an ocular disease, optionally wherein the ocular disease is myopia. 
     
     
         17 . The topical ophthalmological composition of  claim 16 , wherein the topical ophthalmological the composition is adapted to slow a myopia progression.